2. Academic Validation
  3. Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma

Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma

  • Bioorg Med Chem Lett. 2018 Sep 15;28(17):2985-2992. doi: 10.1016/j.bmcl.2018.06.029.
Jean-François Fournier 1,  Yushma Bhurruth-Alcor 2,  Branislav Musicki 2,  Jérome Aubert 2,  Michèle Aurelly 2,  Claire Bouix-Peter 2,  Karinne Bouquet 2,  Laurent Chantalat 2,  Marion Delorme 2,  Bénédicte Drean 2,  Gwenaelle Duvert 2,  Nicolas Fleury-Bregeot 3,  Blanche Gauthier 2,  Karine Grisendi 2,  Craig S Harris 2,  Laurent F Hennequin 2,  Tatiana Isabet 4,  Florence Joly 2,  Guillaume Lafitte 2,  Corinne Millois 2,  Rémy Morgentin 3,  Jonathan Pascau 2,  David Piwnica 2,  Yves Rival 2,  Catherine Soulet 2,  Étienne Thoreau 2,  Loïc Tomas 2
Affiliations

Affiliations

  • 1 Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France. Electronic address: jean-francois.fournier@umontreal.ca.
  • 2 Nestlé Skin Health R&D, 2400 Route des colles, BP 87, 06902 Sophia-Antipolis Cedex, France.
  • 3 Edelris, 115 Avenue Lacassagne, 69003 Lyon, France.
  • 4 Synchrotron Soleil, L'Orme des Merisiers, Saint-Aubin - BP 48, 91192 Gif-sur-Yvette Cedex, France.
PMID: 30122227 DOI: 10.1016/j.bmcl.2018.06.029
Abstract

A series of squaramide-based hydroxamic acids were designed, synthesized and evaluated against human HDAC Enzyme. Squaramides were found to be potent in the Hut78 cell line, but initially suffered from low solubility. Leads with improved solubility and metabolic profiles were shown to be class I, IIB and IV selective.

Keywords

CTCL; HDAC inhibitors; Mycosis fungoides; Squaramide; Topical.

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